Oligopeptides with specific inhibiting properties of...

C - Chemistry – Metallurgy – 07 – K

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530/7.06

C07K 14/78 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1183526

ABSTRACT A process for the preparation of a peptide comprising no more than 10 aminoacids, and including the following sequence: -(N-ter) A-Xl-Gly-Y-Gly-X2-A (C-ter)- wherein: X1 and X2 represent independently of each other a hydroxy- prolyl or a prolyl residue; Y represents either a -Z-X3 or a -X-Z3- residue; X3 represents either a hydroxyprolyl or a prolyl residue; Z represents a spacer aminoacyl residue selected from among dicarboxylic monoaminoacids or monocarboxylic monoaminoacids; and A represents a polyaminoacyl residue, which process comprises either adding the required peptidyl residues step by step, together with the addition and removal of any required protecting groups for the various amino and carboxyl functions, or adding together selected peptidyl residues to pro- vide fragments followed by the condensation together of the frag- ments in an appropriate sequence, together with the addition and removal of any required protecting groups, provided that where fragments are condensed together the reaction does not involve the condensation of a fragment whose C-terminyl residue is either lysyl or glutamic acid. These peptides find use in controlling thrombosis conditions as they exhibit a capacity to inhibit collagen-induced blood platelet aggregation.

377436

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